Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids

We report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue ass...

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Main Authors: Linhu Li, Zhuorong Li, Mingliang Liu, Weiyi Shen, Bin Wang, Huiyuan Guo, Yu Lu
Format: Article
Language:English
Published: MDPI AG 2015-12-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/21/1/49
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author Linhu Li
Zhuorong Li
Mingliang Liu
Weiyi Shen
Bin Wang
Huiyuan Guo
Yu Lu
author_facet Linhu Li
Zhuorong Li
Mingliang Liu
Weiyi Shen
Bin Wang
Huiyuan Guo
Yu Lu
author_sort Linhu Li
collection DOAJ
description We report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue assay (MABA). Although the hybrids are less active than the two reference compounds, the promising activity (MICs: 4 μg/mL) of 2,6-dimethylimidazo[1,2-a]pyridine amide-cinnamamide hybrids 11e and 11k could be a good starting point to further find new lead compounds against multi-drug-resistant tuberculosis.
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spelling doaj.art-74c2c1bcb0da4860b15eca8c9d7c3fe82022-12-21T23:38:36ZengMDPI AGMolecules1420-30492015-12-012114910.3390/molecules21010049molecules21010049Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide HybridsLinhu Li0Zhuorong Li1Mingliang Liu2Weiyi Shen3Bin Wang4Huiyuan Guo5Yu Lu6Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaInstitute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaInstitute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaZhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, ChinaBeijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, ChinaInstitute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaBeijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, ChinaWe report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue assay (MABA). Although the hybrids are less active than the two reference compounds, the promising activity (MICs: 4 μg/mL) of 2,6-dimethylimidazo[1,2-a]pyridine amide-cinnamamide hybrids 11e and 11k could be a good starting point to further find new lead compounds against multi-drug-resistant tuberculosis.http://www.mdpi.com/1420-3049/21/1/49imidazo[1,2-a]pyridine amide-cinnamamide hybridsdesignsynthesisantimycobacterial activity
spellingShingle Linhu Li
Zhuorong Li
Mingliang Liu
Weiyi Shen
Bin Wang
Huiyuan Guo
Yu Lu
Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
Molecules
imidazo[1,2-a]pyridine amide-cinnamamide hybrids
design
synthesis
antimycobacterial activity
title Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
title_full Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
title_fullStr Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
title_full_unstemmed Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
title_short Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
title_sort design synthesis and antimycobacterial activity of novel imidazo 1 2 a pyridine amide cinnamamide hybrids
topic imidazo[1,2-a]pyridine amide-cinnamamide hybrids
design
synthesis
antimycobacterial activity
url http://www.mdpi.com/1420-3049/21/1/49
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